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Pharmacology Flashcards

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1
Q

What are the two active transporters?

A

SLC family and ABC family

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2
Q

What is the ABC transporter?

A

it is a primary active transporter and it uses the ATP-Binding Cassette

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3
Q

what is the SLC transporter?

A

it is a secondary active transporter

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4
Q

what are the examples of SLC transporters?

A

SERT (fluoxetine and serotonin)
DAT (cocaine, methylphenidate, and dopamine)
OATs and OCTs (organic cations and anions)

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5
Q

what is the example of ABC transporter?

A

MDR1/P-glycoprotein receptor

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6
Q

what does MDR1/p-glycoprotein receptor pump out of brain tissue?

A

loperamide (anti-diarrhea)
morphine
HIV protease inhibitors
anticancer drugs

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7
Q

what part of liver cells metabolizes drugs?

A

the smooth ER

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8
Q

what are the phase I reactions?

A

these split the drug - hydrolysis, oxidation, reduction, hydroxylation
and the de’s: dealkylation, deamination, desulfuration, dechlorination

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9
Q

what are the phase II reactions?

A

these conjugate the drugs by adding a substrate:
glucuronide, glycine, glutathione, sulfate, methyl, acetate

*SAM and the 3G’s

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10
Q

what are the other names for cytochrome p450?

A

CYP, monoxygenase, mixed function oxidases

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11
Q

what are the three requirements int eh CYP reaction?

A

NADPH, molecular oxygen, and NADPH-cytochrom P450 reductase

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12
Q

what are the substrates and inducers of CYP1A2?

A

substrates: acetaminophen, caffeine, theophylline, warfarin
inducers: smoking, charcoal, cruciferous vegetables

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13
Q

what are the substrates and inducers of CYP2A6?

A

substrates: warfarin, zidovudine
inducers: none

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14
Q

what are the substrates and inducers of CYP2C9?

A

substrates: hexobarbital, trimethadione, tolbutamide, phenytoin, ibuprofen, s-warfarin
inducers: rifampin, barbiturates

**http is

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15
Q

what are the substrates and inducers of CYP2C19?

A

substrates: diazepam, omeprazole, propanolol
inducers: none

**DOP

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16
Q

what are the substrates for CYP2D6?

A

substrates: amytriptyline, codeine, debrisoquin, fluoxetine, hydrocodone, timolol
inducers: none

**Apollo Caught Deanna For Hera this Time

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17
Q

what are the substrates and inducers for CYP2E1

A

substrates: ethanol and acetaminophen
inducers: ethanol, isoniazid

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18
Q

what are the substrates and inducers for CYP3A4?

A

substrates: cortisol, amiodarone, diazepam, erythromycin, diltiazem, testosterone, triazolam, midazolam, verapamil, nifedipine, progesterone
inducers: barbiturates, glucocorticoids, rifampin, phenytoin

**Carter ADores Eureka Daily
Today They Made Very Nifty Progress

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19
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for glucuronidation?

A

conjugating agent: UDP glucuronic acid
functional groups: OH, COOH, NH2
enzyme: glucuronyl transferase
drugs: morphine, acetaminophen, diazepam, digoxin (MADD)

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20
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for glutathione?

Study These Flashcards
A

conjugating agent: glutathione (GSH)
functional groups: arene oxide, epoxide, halogen, NO2
enzyme: GSH S-transferases
drugs: acetaminophen

21
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for sulfation?

Study These Flashcards
A

conjugating agent: PAPS (3’-phosphoadenosine 5’-phosphosulfate)
functional groups: OH, NH2
enzyme: sulfotransferases
drugs: 3-hydroxycoumarin, acetaminophen, ethanol, 3-hydroxyacetanilide, methydopa

22
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for acetylation?

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A

conjugating agent: acetyl CoA
functional groups: OH, NH2
enzyme: acetyl transferases
drugs: sulfonamide, histamine, isonaizid, procainamide, clonazepam (SHIP C)

23
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for methylation?

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A

conjugating agent: S-adenosylmethionine
functional groups: O, N, S
enzymes: catechol-O-methytransferase, thiopurine-S-methyltransferase, phenol-O-methyltransferase, N-methyltransferase
drugs: thiopurine, carbamzepine epoxide

24
Q

what are three examples of receptors induced by drugs?

Study These Flashcards
A

pregnane X receptor, constitutive androstane receptor, aryl hydrocarbon receptor

25
What drug(s) induce(s) aryl hydrocarbon receptor?
omeprazole
26
What drug(s) induce(s) constitutive androstane receptor?
phenobarbital
27
What drug(s) induce(s) pregnane X receptor?
rifampin, atorvastatin
28
what to penicillin and probenacid do when they interact?
alter elimination
29
what do divalent cations and fluoroquinolones do when they interact?
irritate stomach and impair antibiotic absorption
30
what do EtOH and benzodiazepines do when they interact?
toxic
31
warfarin + aspirin/NSAIDS?
hemorrhagic risk
32
antiseizure drugs and CYP?
if CYP is inhibited, drugs are more effective, if CYP is induced by rifampin, have less effective
33
what do polymorphisms in the CYP2D6 gene cause?
decreased metabolism of debrinoquin
34
what do polymorphisms in the CYP2C19 gene cause?
1. decreased clopidogrel activity (it is a prodrug that requires CYP2C19) 2. increased omeprazole activity (used for gastric ulcers) 3. increased toxicity of phenytoin
35
what do polymorphisms in the CYP2C9 gene cause?
increased activity of S-warfarin, phenyoin, losartan
36
what do polymorphisms in dihydropyrimidine dehydrogenase do?
lead to impaired metabolism of 5-flurouracil which can caused fatal neuro-toxicity in slow metabolizers (non P450 phase I enzyme)
37
what do polymorphisms in pseudocholinesterase do?
dramatically extend the duration of action of succinylcholine (a non P450 phase I enzyme)
38
what does NAT1 do?
N-acetyl transferase 1 acetylates simple aromatic amines
39
what does NAT2 do?
N-acetyl transferase 2 acetylates polycyclic amines and other substrates
40
what does a polymorphism in NAT2 do?
1. causes isoniazid to go down minor pathway and produce neurotoxic product 2. causes procainamide to go down phase I pathways via FMO and produce toxic product 3. faster ANA appearance (Lupus)
41
what does a polymorphism in thiopurine methyl transferase do?
6methylpurine (6MP) goes down different pathways and is coverted to 6-TGN leading to toxicity
42
what does a polymorphism in MDR-1 do?
altered plasma levels of antiretroviral and fexofenadine
43
what does a polymorphism in beta2 adrenergic receptors do?
rapid desensitization by agonists in veins but increased bronchodilator response
44
what does a polymorphism in arachidonate 5-lipoxygenase do?
reduce asthma incidence
45
what does a polymorphism in vitamin K epoxide reductase do?
affects sensitivity to warfarin
46
warfarin metabolism and action?
polymorphisms in CYP2C9 cause slow warfarin metabolism and therefore increase patient sensitivity to warfarin warfarin does its job (anticoagulation) by inhibiting vitamin K epoxide reductase - when VKORC is mutated, warfarin can't bind and inhibit VKORC and no anticoagulative activities
47
inhibitors of CYP450?
macrolide anitbiotics (erythromycin and clarithromycin), antifungals (triazole), ritonavir, fluoxetine, nefasodone, cimetidine
48
what does grapefruit juice inhibit?
CYP3A4

Fundamentals (11 decks)

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